SG188300A1 - Buprenorphine analogs - Google Patents

Buprenorphine analogs Download PDF

Info

Publication number: SG188300A1
Authority: SG; Singapore
Prior art keywords: alkyl; membered; alkoxy; aryl; cycloalkyl
Prior art date: 2010-09-21

Application number

SG2013014113A

Other languages

English (en)

Inventor

Donald J Kyle

Laykea Tafesse

Original Assignee

Purdue Pharma Lp

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2010-09-21

Filing date

2011-09-20

Publication date

2013-04-30

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44903285&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SG188300(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2011-09-20 Application filed by Purdue Pharma Lp filed Critical Purdue Pharma Lp

2013-04-30 Publication of SG188300A1 publication Critical patent/SG188300A1/en

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RMRJXGBAOAMLHD-IHFGGWKQSA-N buprenorphine Chemical class C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)CN2CC1CC1 RMRJXGBAOAMLHD-IHFGGWKQSA-N 0.000 title description 20
150000001875 compounds Chemical class 0.000 claims abstract description 113
-1 Buprenorphine Analog compounds Chemical class 0.000 claims abstract description 32
108010020615 nociceptin receptor Proteins 0.000 claims abstract description 27
208000002193 Pain Diseases 0.000 claims abstract description 17
230000036407 pain Effects 0.000 claims abstract description 14
108090000137 Opioid Receptors Proteins 0.000 claims abstract description 13
206010010774 Constipation Diseases 0.000 claims abstract description 11
125000000217 alkyl group Chemical group 0.000 claims description 3334
125000003545 alkoxy group Chemical group 0.000 claims description 587
229910052684 Cerium Inorganic materials 0.000 claims description 368
125000003118 aryl group Chemical group 0.000 claims description 344
125000003342 alkenyl group Chemical group 0.000 claims description 325
125000000304 alkynyl group Chemical group 0.000 claims description 318
125000000623 heterocyclic group Chemical group 0.000 claims description 285
125000000753 cycloalkyl group Chemical group 0.000 claims description 283
125000001072 heteroaryl group Chemical group 0.000 claims description 238
229910052739 hydrogen Inorganic materials 0.000 claims description 235
239000001257 hydrogen Substances 0.000 claims description 234
125000000392 cycloalkenyl group Chemical group 0.000 claims description 215
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 201
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 197
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 194
229910052799 carbon Inorganic materials 0.000 claims description 133
125000001424 substituent group Chemical group 0.000 claims description 129
150000001602 bicycloalkyls Chemical group 0.000 claims description 89
125000001624 naphthyl group Chemical group 0.000 claims description 62
125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 61
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 57
229940002612 prodrug Drugs 0.000 claims description 44
239000000651 prodrug Substances 0.000 claims description 44
150000003839 salts Chemical class 0.000 claims description 44
239000012453 solvate Substances 0.000 claims description 44
125000002837 carbocyclic group Chemical group 0.000 claims description 33
125000004104 aryloxy group Chemical group 0.000 claims description 32
229910052736 halogen Inorganic materials 0.000 claims description 29
150000002367 halogens Chemical class 0.000 claims description 29
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 27
229910052757 nitrogen Inorganic materials 0.000 claims description 26
125000004433 nitrogen atom Chemical group N* 0.000 claims description 26
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 23
125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 22
229910014585 C2-Ce Inorganic materials 0.000 claims description 20
229910052792 caesium Inorganic materials 0.000 claims description 19
125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 16
102000005962 receptors Human genes 0.000 claims description 15
108020003175 receptors Proteins 0.000 claims description 15
102000003840 Opioid Receptors Human genes 0.000 claims description 12
239000003814 drug Substances 0.000 claims description 10
150000002431 hydrogen Chemical class 0.000 claims description 10
238000001783 near-resonance Rayleigh scattering spectroscopy Methods 0.000 claims description 7
239000000556 agonist Substances 0.000 claims description 6
239000005557 antagonist Substances 0.000 claims description 4
229910052760 oxygen Inorganic materials 0.000 claims description 4
229910052727 yttrium Inorganic materials 0.000 claims description 3
230000009977 dual effect Effects 0.000 claims description 2
125000001475 halogen functional group Chemical group 0.000 claims 157
125000002887 hydroxy group Chemical group [H]O* 0.000 claims 49
QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 18
AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims 11
238000000034 method Methods 0.000 claims 10
DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 6
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical compound C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims 4
125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 3
BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical compound C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 claims 2
FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 claims 2
QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 2
LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 2
YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 2
241000124008 Mammalia Species 0.000 claims 2
YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 2
METKIMKYRPQLGS-UHFFFAOYSA-N atenolol Chemical compound CC(C)NCC(O)COC1=CC=C(CC(N)=O)C=C1 METKIMKYRPQLGS-UHFFFAOYSA-N 0.000 claims 2
125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 2
239000003937 drug carrier Substances 0.000 claims 2
HNQIVZYLYMDVSB-UHFFFAOYSA-N methanesulfonimidic acid Chemical compound CS(N)(=O)=O HNQIVZYLYMDVSB-UHFFFAOYSA-N 0.000 claims 2
239000000546 pharmaceutical excipient Substances 0.000 claims 2
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
125000000446 sulfanediyl group Chemical group *S* 0.000 claims 2
MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 1
RLFBLDXDGTVVAF-KKASODRESA-N (4r,4as,6r,7r,7ar,12bs)-6-((4-(1h-imidazol-1-yl)phenoxy)methyl)-3-(cyclopropylmethyl)-7,9-dimethoxy-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinoline Chemical compound C([C@]12[C@H]3OC=4C(OC)=CC=C(C2=4)C[C@@]2([C@@]11C[C@H](COC=4C=CC(=CC=4)N4C=NC=C4)[C@]3(OC)CC1)[H])CN2CC1CC1 RLFBLDXDGTVVAF-KKASODRESA-N 0.000 claims 1
WMVWSQOJKZZWCI-VTPACTEHSA-N (4r,4as,6r,7r,7ar,12bs)-6-((benzyloxy)methyl)-3-(cyclopropylmethyl)-9-fluoro-7-methoxy-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinoline Chemical compound C([C@]12[C@H]3OC=4C(F)=CC=C(C2=4)C[C@@]2([C@@]11C[C@H](COCC=4C=CC=CC=4)[C@]3(OC)CC1)[H])CN2CC1CC1 WMVWSQOJKZZWCI-VTPACTEHSA-N 0.000 claims 1
CUAYKCKUHHCHSI-RHRQCQTHSA-N (4r,4as,6r,7r,7ar,12bs)-6-((benzyloxy)methyl)-7-methoxy-3-methyl-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinolin-9-amine Chemical compound C([C@@H]1[C@]2(OC)CC[C@]3(C1)[C@@]14[C@H]2OC=2C(N)=CC=C(C4=2)C[C@]3(N(CC1)C)[H])OCC1=CC=CC=C1 CUAYKCKUHHCHSI-RHRQCQTHSA-N 0.000 claims 1
GJUXFJLLYFLPTH-CGRKGAIHSA-N (4r,4as,6s,7r,7ar,12bs)-6-((benzylsulfinyl)methyl)-3-(cyclopropylmethyl)-7,9-dimethoxy-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinoline Chemical compound C([C@]12[C@H]3OC=4C(OC)=CC=C(C2=4)C[C@@]2([C@@]11C[C@H](CS(=O)CC=4C=CC=CC=4)[C@]3(OC)CC1)[H])CN2CC1CC1 GJUXFJLLYFLPTH-CGRKGAIHSA-N 0.000 claims 1
JSYKYDORIGJAKS-BUVWRSTLSA-N (4r,4as,6s,7r,7ar,12bs)-6-((benzylthio)methyl)-3-(cyclopropylmethyl)-7,9-dimethoxy-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinoline Chemical compound C([C@]12[C@H]3OC=4C(OC)=CC=C(C2=4)C[C@@]2([C@@]11C[C@H](CSCC=4C=CC=CC=4)[C@]3(OC)CC1)[H])CN2CC1CC1 JSYKYDORIGJAKS-BUVWRSTLSA-N 0.000 claims 1
FTLHKODYGDDSMC-QXIQULQJSA-N 2-[[(1S,2S,6R,14R,15R,16R)-5-(cyclopropylmethyl)-11,15-dimethoxy-13-oxa-5-azahexacyclo[13.2.2.12,8.01,6.02,14.012,20]icosa-8(20),9,11-trien-16-yl]methylamino]acetic acid Chemical compound C([C@]12[C@H]3OC=4C(OC)=CC=C(C2=4)C[C@@]2([C@@]11C[C@H](CNCC(O)=O)[C@]3(OC)CC1)[H])CN2CC1CC1 FTLHKODYGDDSMC-QXIQULQJSA-N 0.000 claims 1
ADMSKYBLTWMPPO-QGUHJXFESA-N C([C@@H]1[C@]2(OC)CC[C@]3(C1)[C@@]14[C@H]2OC=2C(O)=CC=C(C4=2)C[C@]3(NCC1)[H])OCC1=CC=CC=C1 Chemical compound C([C@@H]1[C@]2(OC)CC[C@]3(C1)[C@@]14[C@H]2OC=2C(O)=CC=C(C4=2)C[C@]3(NCC1)[H])OCC1=CC=CC=C1 ADMSKYBLTWMPPO-QGUHJXFESA-N 0.000 claims 1
VGPKXDDDJZDRDW-NWCUSBOBSA-N C([C@@H]1[C@]2(OC)CC[C@]3(C1)[C@@]14[C@H]2OC=2C(OC)=CC=C(C4=2)C[C@]3(N(CC1)C)[H])OCC1=CC(CCC)=NO1 Chemical compound C([C@@H]1[C@]2(OC)CC[C@]3(C1)[C@@]14[C@H]2OC=2C(OC)=CC=C(C4=2)C[C@]3(N(CC1)C)[H])OCC1=CC(CCC)=NO1 VGPKXDDDJZDRDW-NWCUSBOBSA-N 0.000 claims 1
ULKQZFRXRYHPCM-WNIIMYAPSA-N C([C@@H]1[C@]2(OC)CC[C@]3(C1)[C@@]14[C@H]2OC=2C(OC)=CC=C(C4=2)C[C@]3(N(CC1)C)[H])SC1=NC(C)=NS1 Chemical compound C([C@@H]1[C@]2(OC)CC[C@]3(C1)[C@@]14[C@H]2OC=2C(OC)=CC=C(C4=2)C[C@]3(N(CC1)C)[H])SC1=NC(C)=NS1 ULKQZFRXRYHPCM-WNIIMYAPSA-N 0.000 claims 1
UOHHELYULJAZBW-NPBSHTHCSA-N C([C@@H]1[C@]2(OC)CC[C@]3(C1)[C@@]14[C@H]2OC=2C(OC)=CC=C(C4=2)C[C@]3(N(CC1)CCC(N)=O)[H])OCC1=CC=CC=C1 Chemical compound C([C@@H]1[C@]2(OC)CC[C@]3(C1)[C@@]14[C@H]2OC=2C(OC)=CC=C(C4=2)C[C@]3(N(CC1)CCC(N)=O)[H])OCC1=CC=CC=C1 UOHHELYULJAZBW-NPBSHTHCSA-N 0.000 claims 1
JIKNKSSGOZQLQU-NPBSHTHCSA-N C([C@@H]1[C@]2(OC)CC[C@]3(C1)[C@@]14[C@H]2OC=2C(OC)=CC=C(C4=2)C[C@]3(N(CC1)CCC(O)=O)[H])OCC1=CC=CC=C1 Chemical compound C([C@@H]1[C@]2(OC)CC[C@]3(C1)[C@@]14[C@H]2OC=2C(OC)=CC=C(C4=2)C[C@]3(N(CC1)CCC(O)=O)[H])OCC1=CC=CC=C1 JIKNKSSGOZQLQU-NPBSHTHCSA-N 0.000 claims 1
FDYCYWQDIVTVDR-RHRQCQTHSA-N C([C@@H]1[C@]2(OC)CC[C@]3(C1)[C@@]14[C@H]2OC=2C(OC)=CC=C(C4=2)C[C@]3(NCC1)[H])OCC1=CC=CC=C1 Chemical compound C([C@@H]1[C@]2(OC)CC[C@]3(C1)[C@@]14[C@H]2OC=2C(OC)=CC=C(C4=2)C[C@]3(NCC1)[H])OCC1=CC=CC=C1 FDYCYWQDIVTVDR-RHRQCQTHSA-N 0.000 claims 1
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229960003406 levorphanol Drugs 0.000 description 1
230000004060 metabolic process Effects 0.000 description 1
JVLBPIPGETUEET-GAAHOAFPSA-O methylnaltrexone Chemical compound C[N+]1([C@@H]2CC=3C4=C(C(=CC=3)O)O[C@@H]3[C@]4([C@@]2(O)CCC3=O)CC1)CC1CC1 JVLBPIPGETUEET-GAAHOAFPSA-O 0.000 description 1
OPKAGVRBWHZYKM-UHFFFAOYSA-N n-methyl-n-methylsulfonylmethanesulfonamide Chemical compound CS(=O)(=O)N(C)S(C)(=O)=O OPKAGVRBWHZYKM-UHFFFAOYSA-N 0.000 description 1
229960002009 naproxen Drugs 0.000 description 1
CMWTZPSULFXXJA-VIFPVBQESA-M naproxen(1-) Chemical compound C1=C([C@H](C)C([O-])=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-M 0.000 description 1
208000004296 neuralgia Diseases 0.000 description 1
208000021722 neuropathic pain Diseases 0.000 description 1
229940121367 non-opioid analgesics Drugs 0.000 description 1
239000003401 opiate antagonist Substances 0.000 description 1
230000008520 organization Effects 0.000 description 1
229940051877 other opioids in atc Drugs 0.000 description 1
229960005118 oxymorphone Drugs 0.000 description 1
229960005489 paracetamol Drugs 0.000 description 1
239000004031 partial agonist Substances 0.000 description 1
210000002509 periaqueductal gray Anatomy 0.000 description 1
231100000857 poor renal function Toxicity 0.000 description 1
102000004196 processed proteins & peptides Human genes 0.000 description 1
230000001105 regulatory effect Effects 0.000 description 1
238000003571 reporter gene assay Methods 0.000 description 1
238000012552 review Methods 0.000 description 1
230000000638 stimulation Effects 0.000 description 1
239000000126 substance Substances 0.000 description 1
208000024891 symptom Diseases 0.000 description 1
208000011580 syndromic disease Diseases 0.000 description 1
238000012360 testing method Methods 0.000 description 1
230000001225 therapeutic effect Effects 0.000 description 1
231100000027 toxicology Toxicity 0.000 description 1
230000001960 triggered effect Effects 0.000 description 1
FQCQGOZEWWPOKI-UHFFFAOYSA-K trisalicylate-choline Chemical compound [Mg+2].C[N+](C)(C)CCO.OC1=CC=CC=C1C([O-])=O.OC1=CC=CC=C1C([O-])=O.OC1=CC=CC=C1C([O-])=O FQCQGOZEWWPOKI-UHFFFAOYSA-K 0.000 description 1
239000002023 wood Substances 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
- C07D489/09—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems
- C07D489/10—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14
- C07D489/12—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Public Health (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Pharmacology & Pharmacy (AREA)
Veterinary Medicine (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Pain & Pain Management (AREA)
Rheumatology (AREA)
Biomedical Technology (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

SG2013014113A 2010-09-21 2011-09-20 Buprenorphine analogs SG188300A1 (en)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US38491210P	2010-09-21	2010-09-21
US201161503674P	2011-07-01	2011-07-01
PCT/IB2011/002208 WO2012038813A1 (en)	2010-09-21	2011-09-20	Buprenorphine analogs

Publications (1)

Publication Number	Publication Date
SG188300A1 true SG188300A1 (en)	2013-04-30

Family

ID=44903285

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SG2013014113A SG188300A1 (en)	2010-09-21	2011-09-20	Buprenorphine analogs

Country Status (34)

Country	Link
US (1)	US9221831B2 (es)
EP (1)	EP2619212B1 (es)
JP (2)	JP5977240B2 (es)
KR (2)	KR20150027315A (es)
CN (2)	CN103154000A (es)
AR (1)	AR083062A1 (es)
AU (1)	AU2011306644B2 (es)
CA (1)	CA2810356C (es)
CL (1)	CL2013000732A1 (es)
CO (1)	CO6690803A2 (es)
CR (1)	CR20130129A (es)
CY (1)	CY1117227T1 (es)
DK (1)	DK2619212T3 (es)
DO (1)	DOP2013000060A (es)
EA (1)	EA201390422A1 (es)
EC (1)	ECSP13012543A (es)
ES (1)	ES2566828T3 (es)
HR (1)	HRP20160281T1 (es)
HU (1)	HUE027195T2 (es)
ME (1)	ME02367B (es)
MX (1)	MX2013003354A (es)
NI (1)	NI201300032A (es)
NZ (1)	NZ609200A (es)
PE (1)	PE20140020A1 (es)
PH (1)	PH12013500530A1 (es)
PL (1)	PL2619212T3 (es)
RS (1)	RS54579B1 (es)
SG (1)	SG188300A1 (es)
SI (1)	SI2619212T1 (es)
SM (1)	SMT201600088B (es)
TW (2)	TW201242968A (es)
UY (1)	UY33618A (es)
WO (1)	WO2012038813A1 (es)
ZA (1)	ZA201301217B (es)

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2011
- 2011-09-20 ES ES11776855.6T patent/ES2566828T3/es active Active
- 2011-09-20 RS RS20160119A patent/RS54579B1/sr unknown
- 2011-09-20 KR KR20157004529A patent/KR20150027315A/ko not_active Withdrawn
- 2011-09-20 CN CN2011800450775A patent/CN103154000A/zh active Pending
- 2011-09-20 PL PL11776855.6T patent/PL2619212T3/pl unknown
- 2011-09-20 ME MEP-2016-38A patent/ME02367B/me unknown
- 2011-09-20 CN CN201510733006.4A patent/CN105399751A/zh active Pending
- 2011-09-20 SG SG2013014113A patent/SG188300A1/en unknown
- 2011-09-20 UY UY0001033618A patent/UY33618A/es unknown
- 2011-09-20 AR ARP110103431A patent/AR083062A1/es unknown
- 2011-09-20 NZ NZ609200A patent/NZ609200A/en not_active IP Right Cessation
- 2011-09-20 US US13/825,241 patent/US9221831B2/en active Active
- 2011-09-20 EP EP11776855.6A patent/EP2619212B1/en active Active
- 2011-09-20 JP JP2013529723A patent/JP5977240B2/ja not_active Expired - Fee Related
- 2011-09-20 EA EA201390422A patent/EA201390422A1/ru unknown
- 2011-09-20 DK DK11776855.6T patent/DK2619212T3/en active
- 2011-09-20 PE PE2013000548A patent/PE20140020A1/es not_active Application Discontinuation
- 2011-09-20 HU HUE11776855A patent/HUE027195T2/en unknown
- 2011-09-20 AU AU2011306644A patent/AU2011306644B2/en not_active Ceased
- 2011-09-20 CA CA2810356A patent/CA2810356C/en not_active Expired - Fee Related
- 2011-09-20 HR HRP20160281TT patent/HRP20160281T1/hr unknown
- 2011-09-20 KR KR1020137009943A patent/KR101630912B1/ko not_active Expired - Fee Related
- 2011-09-20 PH PH1/2013/500530A patent/PH12013500530A1/en unknown
- 2011-09-20 MX MX2013003354A patent/MX2013003354A/es not_active Application Discontinuation
- 2011-09-20 WO PCT/IB2011/002208 patent/WO2012038813A1/en not_active Ceased
- 2011-09-20 SI SI201130750T patent/SI2619212T1/sl unknown
- 2011-09-21 TW TW100133950A patent/TW201242968A/zh unknown
- 2011-09-21 TW TW102147960A patent/TW201422621A/zh unknown
2013
- 2013-02-18 ZA ZA2013/01217A patent/ZA201301217B/en unknown
- 2013-03-18 CL CL2013000732A patent/CL2013000732A1/es unknown
- 2013-03-20 NI NI201300032A patent/NI201300032A/es unknown
- 2013-03-20 DO DO2013000060A patent/DOP2013000060A/es unknown
- 2013-03-21 CR CR20130129A patent/CR20130129A/es not_active Application Discontinuation
- 2013-04-05 EC ECSP13012543 patent/ECSP13012543A/es unknown
- 2013-04-18 CO CO13100225A patent/CO6690803A2/es unknown
2015
- 2015-11-19 JP JP2015226945A patent/JP2016102115A/ja not_active Withdrawn
2016
- 2016-03-04 CY CY20161100187T patent/CY1117227T1/el unknown
- 2016-03-24 SM SM201600088T patent/SMT201600088B/xx unknown

Also Published As

Publication number	Publication date
ME02367B (me)	2016-06-20
US9221831B2 (en)	2015-12-29
AU2011306644B2 (en)	2015-07-02
CO6690803A2 (es)	2013-06-17
JP2016102115A (ja)	2016-06-02
ZA201301217B (en)	2013-09-25
DOP2013000060A (es)	2013-04-30
CN103154000A (zh)	2013-06-12
TW201422621A (zh)	2014-06-16
CN105399751A (zh)	2016-03-16
AR083062A1 (es)	2013-01-30
NI201300032A (es)	2014-01-13
NZ609200A (en)	2015-01-30
PH12013500530A1 (en)	2017-08-09
US20140057931A1 (en)	2014-02-27
HRP20160281T1 (hr)	2016-04-08
ES2566828T3 (es)	2016-04-15
EP2619212B1 (en)	2016-01-06
CA2810356C (en)	2016-06-14
EP2619212A1 (en)	2013-07-31
KR20130097210A (ko)	2013-09-02
CL2013000732A1 (es)	2013-07-26
PE20140020A1 (es)	2014-01-31
MX2013003354A (es)	2013-06-24
HUE027195T2 (en)	2016-10-28
DK2619212T3 (en)	2016-03-21
TW201242968A (en)	2012-11-01
CY1117227T1 (el)	2017-04-05
KR101630912B1 (ko)	2016-06-15
AU2011306644A1 (en)	2013-04-11
SI2619212T1 (sl)	2016-04-29
UY33618A (es)	2012-03-30
SMT201600088B (it)	2016-04-29
CA2810356A1 (en)	2012-03-29
JP2013543488A (ja)	2013-12-05
KR20150027315A (ko)	2015-03-11
ECSP13012543A (es)	2013-06-28
HK1187045A1 (en)	2014-03-28
PL2619212T3 (pl)	2016-09-30
RS54579B1 (sr)	2016-06-30
WO2012038813A1 (en)	2012-03-29
CR20130129A (es)	2013-08-29
EA201390422A1 (ru)	2014-01-30
JP5977240B2 (ja)	2016-08-24

Publication	Publication Date	Title
EP2619212B1 (en)	2016-01-06	Buprenorphine analogs as opioid receptor agonists and/or antagonists
AU2009277095B2 (en)	2012-09-06	Buprenorphine analogs
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